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Bioorg Med Chem Lett. 2010 Jan 1;20(1):112-6. doi: 10.1016/j.bmcl.2009.11.013. Epub 2009 Nov 12.

Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.

Author information

1
Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd, 403, Yoshino-Cho 1-Chome, Kita-Ku, Saitama-Shi, Saitama 331-9530, Japan. tetsuo.takayama@po.rd.taisho.co.jp

Abstract

We have identified a novel series of ring-fused pyrazole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC(50)s <1nM) as well as excellent cellular activity against mixed lymphocyte reaction (MLR) (IC(50)s <1nM).

PMID:
19945867
DOI:
10.1016/j.bmcl.2009.11.013
[Indexed for MEDLINE]

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